Topical and transdermal administration of peptidyl drugs using hydroxide releasing agents as permeation enhancers
OwnerEric C. Luo, Tsung-Min Hsuinventors
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Abstract
A method is provided for increasing the permeability of skin or mucosal tissue to a topically or transdermally administered pharmacologically or cosmeceutically active peptide, polypeptide or protein. The method involves use of a specified amount of a hydroxide-releasing agent, the amount optimized to increase the flux of the peptide, polypeptide or protein through a body surface while minimizing the likelihood of skin damage, irritation or sensitization. Formulations and drug delivery devices employing hydroxide-releasing agents as permeation enhancers are provided as well.
Claims68
A composition of matter useful for the delivery of a peptidyl drug through a body surface, comprising:
- (a) a therapeutically effective amount of a peptidyl drug;
- (b) a hydroxide-releasing agent in an amount effective to enhance the flux of the peptidyl drug through the body surface without causing damage thereto and effective to provide a pH in the range of approximately 8.0 to 13 at the localized region of the body surface during drug administration;
- and wherein the amount of hydroxide-releasing agent in the composition is the total of (a) the amount required to neutralize any acidic species in the composition plus (b) an amount equal to approximately 0.25 wt. % to 25.0 wt. % of the composition;
- and
- (c) a pharmaceutically acceptable carrier suitable for topical or transdermal peptidyl drug administration.
A system for the topical or transdermal administration of a peptidyl drug, comprising:
- (a) at least one drug reservoir containing the peptidyl drug and a hydroxide-releasing agent in an amount effective to enhance the flux of the drug through the body surface without causing damage thereto and effective to provide a pH in the range of approximately 8.0 to 13 at the localized region of the body surface during drug administration;
- and wherein the amount of hydroxide-releasing agent in the reservoir is the total of (a) the amount required to neutralize any acidic species in the reservoir plus (b) an amount equal to approximately 0.25 wt. % to 25.0 wt. % of the reservoir;
- (b) a means for maintaining the system in drug and enhancer transmitting relationship to the body surface;
- and
- (c) a backing layer that serves as the outer surface of the device during use.
Dependencies are inferred from the claim text.